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RU2007134564A - HIV INHIBITING DERIVATIVES OF 2- (4-CYANOPHENYLAMINO) -PYRIMIDINE OXIDE - Google Patents

HIV INHIBITING DERIVATIVES OF 2- (4-CYANOPHENYLAMINO) -PYRIMIDINE OXIDE Download PDF

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Publication number
RU2007134564A
RU2007134564A RU2007134564/04A RU2007134564A RU2007134564A RU 2007134564 A RU2007134564 A RU 2007134564A RU 2007134564/04 A RU2007134564/04 A RU 2007134564/04A RU 2007134564 A RU2007134564 A RU 2007134564A RU 2007134564 A RU2007134564 A RU 2007134564A
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RU
Russia
Prior art keywords
cyanophenylamino
compound according
pyrimidine oxide
hiv inhibiting
inhibiting derivatives
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Application number
RU2007134564/04A
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Russian (ru)
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RU2398768C2 (en
Inventor
КОК Херман Аугустинус ДЕ (BE)
Кок Херман Аугустинус Де
Пит Том Берт Поль ВИГЕРИНК (BE)
Пит Том Берт Поль Вигеринк
Original Assignee
Тиботек Фарммасьютикалз Лтд. (Ie)
Тиботек Фарммасьютикалз Лтд.
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Publication of RU2007134564A publication Critical patent/RU2007134564A/en
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Publication of RU2398768C2 publication Critical patent/RU2398768C2/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Virology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Medicinal Chemistry (AREA)
  • Communicable Diseases (AREA)
  • AIDS & HIV (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Claims (6)

1. Соединение формулы:1. The compound of the formula:
Figure 00000001
Figure 00000001
 его фармацевтически приемлемая аддитивная соль или его стереохимически изомерная форма, гдеits pharmaceutically acceptable additive salt or its stereochemically isomeric form, where R1 представляет собой атом галогена;R 1 represents a halogen atom; R2 и R3 каждый независимо друг от друга представляет собой С1-6-алкил.R 2 and R 3 each independently of one another is C 1-6 alkyl. 2. Соединение по п.1, где R1 представляет собой атом хлора или брома.2. The compound according to claim 1, where R 1 represents a chlorine or bromine atom. 3. Соединение по п.1, где R1 представляет собой атом брома.3. The compound according to claim 1, where R 1 represents a bromine atom. 4. Соединение по любому из пп.1-3, где R2 и R3 представляют собой метил.4. The compound according to any one of claims 1 to 3, where R 2 and R 3 are methyl. 5. Фармацевтическая композиция, содержащая фармацевтически приемлемый носитель и в качестве активного ингредиента терапевтически эффективное количество соединения по любому из пп.1-4.5. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and, as an active ingredient, a therapeutically effective amount of a compound according to any one of claims 1 to 4. 6. Способ получения композиции по п.5, включающий тщательное смешение активного ингредиента и носителя. 6. A method of obtaining a composition according to claim 5, comprising carefully mixing the active ingredient and the carrier.
RU2007134564/04A 2005-02-18 2006-02-20 Hiv-inhibiting 2-(4-cyanophenylamino)-pyrimidine-oxide derivatives RU2398768C2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP05101270.6 2005-02-18
EP05101270 2005-02-18

Publications (2)

Publication Number Publication Date
RU2007134564A true RU2007134564A (en) 2009-03-27
RU2398768C2 RU2398768C2 (en) 2010-09-10

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RU2007134564/04A RU2398768C2 (en) 2005-02-18 2006-02-20 Hiv-inhibiting 2-(4-cyanophenylamino)-pyrimidine-oxide derivatives

Country Status (10)

Country Link
US (1) US7935711B2 (en)
EP (1) EP1853567B1 (en)
JP (1) JP5247154B2 (en)
CN (1) CN101119976B (en)
AU (1) AU2006215599B2 (en)
BR (1) BRPI0607811B8 (en)
ES (1) ES2533258T3 (en)
MX (1) MX2007010051A (en)
RU (1) RU2398768C2 (en)
WO (1) WO2006087387A1 (en)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2089384B1 (en) 2006-12-13 2015-08-05 F. Hoffmann-La Roche AG 2-(piperidin-4-yl)-4-phenoxy-or phenylamino-pyrimidine derivatives as non-nucleoside reverse transcriptase inhibitors
US20110196156A1 (en) * 2009-06-22 2011-08-11 Mukund Keshav Gurjar Process for synthesis of diarylpyrimidine non-nucleoside reverse transcriptase inhibitor
WO2011017079A1 (en) 2009-07-27 2011-02-10 Teva Pharmaceutical Industries Ltd. Process for the preparation and purification of etravirine and intermediates thereof
CN102648197A (en) * 2009-08-12 2012-08-22 铂雅制药公司 Method of promoting apoptosis and inhibiting metastasis
CA2803848A1 (en) * 2010-06-28 2012-01-05 Hetero Research Foundation A process for etravirine intermediate and polymorphs of etravirine
NZ604583A (en) 2010-06-29 2015-04-24 Verastem Inc Oral formulations of kinase inhibitors
JP5923499B2 (en) 2010-06-30 2016-05-24 ベラステム インコーポレイテッド Synthesis and use of kinase inhibitors
US9126949B2 (en) 2011-04-25 2015-09-08 Hetero Research Foundation Process for rilpivirine
PT2702045T (en) * 2011-04-26 2018-01-11 Mylan Laboratories Ltd Novel process for the preparation of etravirine
CA3158698A1 (en) 2020-02-19 2021-08-26 Alexander Vitalievich Kurkin Pyrimidine-based bicycles as antiviral agents for the treatment and prevention of hiv infection

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU227453B1 (en) * 1998-11-10 2011-06-28 Janssen Pharmaceutica Nv Hiv replication inhibiting pyrimidines, and pharmaceutical compositions containing them
WO2001022938A1 (en) * 1999-09-24 2001-04-05 Janssen Pharmaceutica N.V. Antiviral compositions
AR039540A1 (en) * 2002-05-13 2005-02-23 Tibotec Pharm Ltd MICROBICIDE COMPOUNDS WITH PIRIMIDINE OR TRIAZINE CONTENT
TW200409629A (en) * 2002-06-27 2004-06-16 Bristol Myers Squibb Co 2,4-disubstituted-pyridine N-oxides useful as HIV reverse transcriptase inhibitors
ES2380631T3 (en) * 2004-09-30 2012-05-17 Tibotec Pharmaceuticals HIV-substituted 5-position substituted pyrimidines
BRPI0516746A (en) * 2004-09-30 2008-09-23 Tibotec Pharm Ltd 5-heterocyclyl pyrimidines for hiv inhibition
CN101107234B (en) * 2005-01-27 2013-06-19 泰博特克药品有限公司 HIV inhibiting 2-(4-cyanophenylamino) pyrimidine derivatives
PL1858861T3 (en) * 2005-03-04 2010-12-31 Janssen Sciences Ireland Uc Hiv inhibiting 2-(4-cyanophenyl)-6-hydroxylaminopyrimidines
DE602007009508D1 (en) * 2006-03-30 2010-11-11 Little Island Co Cork HIV-INHIBITED 5- (HYDROXYMETHYLENE AND AMINOMETHYLENE) SUBSTITUTED PYRIMIDINES
MX2008012576A (en) * 2006-03-30 2008-10-10 Tibotec Pharm Ltd Hiv inhibiting 5-amido substituted pyrimidines.
CA2674178C (en) * 2006-12-29 2015-11-10 Tibotec Pharmaceuticals Ltd. Hiv inhibiting 6-substituted pyrimidines

Also Published As

Publication number Publication date
AU2006215599B2 (en) 2012-09-27
RU2398768C2 (en) 2010-09-10
ES2533258T3 (en) 2015-04-08
CN101119976B (en) 2010-12-22
BRPI0607811A2 (en) 2009-10-06
WO2006087387A1 (en) 2006-08-24
MX2007010051A (en) 2007-09-21
US20080194602A1 (en) 2008-08-14
CN101119976A (en) 2008-02-06
EP1853567A1 (en) 2007-11-14
US7935711B2 (en) 2011-05-03
EP1853567B1 (en) 2014-12-31
BRPI0607811B8 (en) 2021-05-25
AU2006215599A1 (en) 2006-08-24
JP5247154B2 (en) 2013-07-24
JP2008530184A (en) 2008-08-07
BRPI0607811B1 (en) 2019-08-20

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Effective date: 20161128